Inhibitors of protein methyltransferases and demethylases

HU Kaniskan, ML Martini, J Jin - Chemical reviews, 2018 - ACS Publications
Post-translational modifications of histones by protein methyltransferases (PMTs) and
histone demethylases (KDMs) play an important role in the regulation of gene expression …

Pharmacological inhibition of LSD1 for cancer treatment

GJ Yang, PM Lei, SY Wong, DL Ma, CH Leung - Molecules, 2018 - mdpi.com
Lysine-specific demethylase 1A (LSD1, also named KDM1A) is a demethylase that can
remove methyl groups from histones H3K4me1/2 and H3K9me1/2. It is aberrantly expressed …

LSD1 activates a lethal prostate cancer gene network independently of its demethylase function

A Sehrawat, L Gao, Y Wang… - Proceedings of the …, 2018 - National Acad Sciences
Medical castration that interferes with androgen receptor (AR) function is the principal
treatment for advanced prostate cancer. However, clinical progression is universal, and …

Targeting the senescence-overriding cooperative activity of structurally unrelated H3K9 demethylases in melanoma

Y Yu, K Schleich, B Yue, S Ji, P Lohneis, K Kemper… - Cancer cell, 2018 - cell.com
Oncogene-induced senescence, eg, in melanocytic nevi, terminates the expansion of pre-
malignant cells via transcriptional silencing of proliferation-related genes due to decoration …

Epigenetics in ovarian cancer: premise, properties, and perspectives

Q Yang, Y Yang, N Zhou, K Tang, WB Lau, B Lau… - Molecular cancer, 2018 - Springer
Malignant ovarian tumors bear the highest mortality rate among all gynecological cancers.
Both late tumor diagnosis and tolerance to available chemical therapy increase patient …

Epigenetic targeting of glioblastoma

M Romani, MP Pistillo, B Banelli - Frontiers in oncology, 2018 - frontiersin.org
Glioblastoma is one of the first tumors where the biological changes accompanying a single
epigenetic modification, the methylation of the MGMT gene, were found to be of clinical …

Lysine-specific demethylase 1A as a promising target in acute myeloid leukemia

D Magliulo, R Bernardi, S Messina - Frontiers in Oncology, 2018 - frontiersin.org
Acute myeloid leukemia (AML) is a heterogeneous hematopoietic malignancy characterized
by the accumulation of incompletely differentiated progenitor cells (blasts) in the bone …

LSD1 inhibition prolongs survival in mouse models of MPN by selectively targeting the disease clone

JS Jutzi, M Kleppe, J Dias, HF Staehle, K Shank… - …, 2018 - journals.lww.com
Despite recent advances, the myeloproliferative neoplasms (MPNs) are attended by
considerable morbidity and mortality. Janus kinase (Jak) inhibitors such as ruxolitinib …

LSD1 coordinates with the SIN3A/HDAC complex and maintains sensitivity to chemotherapy in breast cancer

Y Yang, W Huang, R Qiu, R Liu, Y Zeng… - Journal of Molecular …, 2018 - academic.oup.com
Abstract Lysine-specific demethylase 1 (LSD1) was the first histone demethylase identified
as catalysing the removal of mono-and di-methylation marks on histone H3-K4. Despite the …

KDM1A microenvironment, its oncogenic potential, and therapeutic significance

T Ismail, HK Lee, C Kim, T Kwon, TJ Park… - Epigenetics & …, 2018 - Springer
The lysine-specific histone demethylase 1A (KDM1A) was the first demethylase to challenge
the concept of the irreversible nature of methylation marks. KDM1A, containing a flavin …